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基于生物电子等排和活性亚结构拼接原理,设计合成了16个结构新颖,含噁二唑结构的甲氧基丙烯酸酯类杀菌剂,化合物结构均已通过核磁共振氢谱、碳谱和高分辨质谱确证,并对其进行了离体杀菌活性测试.结果表明:部分化合物对于油菜菌核病菌的活性与对照药嘧菌酯相当,部分化合物对于小麦纹枯病菌活性超过对照药嘧菌酯.进行了初步的构效关系研究.(E)-2-{2-[4-(噁二唑-2-基)苯基硫甲基]苯基}-3-甲氧基丙烯酸甲酯(IIa)和(E)-2-{2-[4-(5-乙基噁二唑-2-基)苯基硫甲基]苯基}-3-甲氧基丙烯酸甲酯(IIc)对于多种真菌表现很好的抑制活性,可作为先导化合物进一步研究.
Based on the principle of bioisostere and active sub-structure splicing, 16 novel and functional oxadiazole-containing bactericides were designed and synthesized. The structures of these compounds have been confirmed by 1H NMR, GC and HR The results of mass spectrometry and in vitro bactericidal activity test showed that some of the compounds showed comparable activity to the control azoxystrobin, while some of the compounds showed more activity against the wheat sheath blight than the control azoxystrobin. (E) -2- (2- [4- (oxadiazol-2-yl) phenylthiomethyl] phenyl} -3-methoxyacrylate (IIa ) And methyl (E) -2- {2- [4- (5-ethyloxadiazol-2-yl) phenylthiomethyl] phenyl} Species fungi showed good inhibitory activity and could be further studied as lead compounds.